SAR7334

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Chemical Structure| 1333210-07-3 同义名 : CPA-1588
CAS号 : 1333210-07-3
货号 : A433794
分子式 : C21H22ClN3O
纯度 : 95%
分子量 : 367.87
MDL号 : MFCD27992059
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 300 mg/mL(815.5 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 The cation channel transient receptor potential canonical (TRPC) 6 has been associated with several pathologies including focal segmental glomerulosclerosis, pulmonary hypertension and ischaemia reperfusion-induced lung oedema. SAR7334 inhibited TRPC6, TRPC3 and TRPC7-mediated Ca2+ influx into cells with IC50s of 9.5, 282 and 226 nM. SAR7334 dose-dependently reduces TRPC6 currents with an IC50 of 7.9 nM. In most TRPC6-HEK-FITR cells, trypsin evoked large, rapidly declining TRPC6 currents that reached an almost steady-state level within 30–60 s. This current was substantially reduced by 100 nM SAR7334. The reduction of trypsin-induced TRPC6 currents by 100 nM SAR7334 amounted to 88 ± 3% (n = 5). In perfused isolated lungs from mice, SAR7334 abolished hypoxia-induced increases in pulmonary arterial pressure. Half maximal inhibition was achieved at about 100 nM indicating that SAR7334 is able to efficiently block native TRPC6 channels in situ[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.72mL

0.54mL

0.27mL

13.59mL

2.72mL

1.36mL

27.18mL

5.44mL

2.72mL
参考文献

[1]Ilatovskaya DV, Palygin O, et al. The Role of Angiotensin II in Glomerular Volume Dynamics and Podocyte Calcium Handling. Sci Rep. 2017 Mar 22;7(1):299.

[2]Maier T, Follmann M, et al. Discovery and pharmacological characterization of a novel potent inhibitor of diacylglycerol-sensitive TRPC cation channels. Br J Pharmacol. 2015 Jul;172(14):3650-60.

[3]Maier T, Follmann M, Hessler G, et al. Discovery and pharmacological characterization of a novel potent inhibitor of diacylglycerol-sensitive TRPC cation channels. Br J Pharmacol. 2015;172(14):3650‐3660